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Quantification of flupirtine maleate polymorphs using X-ray powder diffraction

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Chinese Chemical Letters 2016年第11期27卷 1666-1672页

作者： Yu-Mei Zhao Zhi-Bing Zheng Song Li laboratory of Computer-Aided Drug Design & Discovery Beijing Institute of Pharmacology and Toxicology laboratory of Structure Identification Beijing Institute of Pharmacology and Toxicology State key laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and Toxicology

Flupirtine maleate, a pharmaceutical compound for treating psychotic disease in clinics, has seven polymorphs. Form A, with better crystal stability and bioavailability, has been widely used as the pharmaceutical crystal form. Unfortunately, it is usually found in a polymorphic mixture with form B. In this study, pure crystal forms of A and B were prepared and characterized by X-ray powder diffraction （XRPD）, Fourier transform infrared spectroscopy （FT-IR） and thermal analysis. An XRPD-based method for the quantitative determination of the amount of the flupirtine maleate polymorphs form A and form B was also established through a systematic optimization of instrumental parameters. The results of the analytical methodology validation showed that the XPRD method had a broad quantitative range of 0- 100% （w/w）, good linear relationship, with R2= 0.999, excellent repeatability and precision and low limits of detection （LoD） of 0.15% （w/w） and quantification （LoQ） of 0.5% （w/w）. The results also showed that the single-peak method was not as good as the whole pattern in reducing the influence of the preferred orientation, but this can be compensated for by a systematic optimization of instrumental parameters and validating the analytical methodology to reduce errors and obtain a good, repeatable, sensitive, and accurate method. This XRPD method can be used to analyze mixtures of flupirtine maleate polymorphs （forms A and B） quantitatively and control the quality of the bulk drug.

关键词： Flupirtine maleate X-ray powder diffraction Quantitative analysis of polymorphs Preferred orientation Transmission

Characteristics of the traditional Liu-Wei-Di-Huang prescription reassessed in modern pharmacology

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Chinese Journal of Natural Medicines 2019年第2期17卷 103-121页

作者： CHENG Xiao-Rui QI Chun-Hui WANG Tong-Xing ZHOU Wen-Xia ZHANG Yong-Xiang Academy of Military Medical Science Institute of Pharmacology and Toxicology State key laboratory of toxicology and Medical Countermeasures

Liu-Wei-Di-Huang(LW) is a Yin nourishing and kidney tonifying prescription in traditional Chinese medicine with promising pharmacological characteristics that can be further exploited and developed in modern medicine. We provide a comprehensive and detailed literature report on the clinical and experimental pharmacology of LW,including its quality control parameters, phytochemistry, pharmacokinetics, and toxicology. Our literature review indicates that the LW prescription possesses a unique combination of pharmacological characteristics that can be safely used for treating very different diseases. Quality control and pharmacokinetic parameters of LW are mostly based on its major bioactive phytochemical constituents. We postulate that modulating or rebalancing the neuroendocrine immunomodulation network in the body is the underlying mechanism of the multiple pharmacological activities displayed by LW.

关键词： Liu-Wei-Di-Huang Traditional Chinese medicine Pharmacology Phytochemistry Pharmacokinetics toxicology

Dynamic changes of serum protein in rats with acute intoxication of Chinese cobra snake venom by proteomic analysis

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forensic Sciences Research 2020年第4期5卷 309-321页

作者： Hui Yan Ping Xiang Jingshuo Zhang Liqi Xie Min Shen Shanghai key laboratory of forensic Science Shanghai Forensic PlatformDepartment of Forensic ToxicologyAcademy of Forensic ScienceShanghaiChina College of Pharmaceutical Sciences Soochow UniverstitySuzhouJiangsuChina Institutes of Biomedical Sciences Fudan UniversityShanghaiChina

To elucidate the toxic mechanism of snake venom at the protein level,proteomics technol-ogy was applied to investigate the effect of venom on circulation in the mammalian *** proteomic analysis was performed to profile the dynamic changes in the sera of Sprague-Dawley rats administered with Chinese cobra venom or *** 8-plex iTRAQ analysis,392 and 636 serum proteins were identified to be linearly upregulated or downre-gulated over time in the low-dose group and high-dose group,*** proteins were mainly associated with the acute phase response pathway,complement system,and liver X receptor(LXR)/retinoid X receptor(RXR)and farnesoid X receptor(FXR)/RXR activation *** with the low-dose group,the immune response and integrin pathways were inhibited in the high-dose group,although no obvious effect was *** con-sistently higher or lower expression in the high-dose group compared to the low-dose group throughout the whole process of venom poisoning,two proteins,Kininogen-1(KNG1)and orosomucoid 1(ORM1),which are involved in metabolism and immune response,occu-pied a core position in the pathway network and are considered venom dose-dependent biomarker candidates.

关键词： forensic sciences forensic toxicology proteomics snake bite cobra serum rats

Screening for volatile sulphur compounds in a fatal accident case

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forensic Sciences Research 2017年第4期2卷 192-197页

作者： Ping Xiang Huosheng Qiang Baohua Shen Min Shen Department of forensic toxicology Shanghai Key Laboratory of Forensic MedicineShanghai Forensic Service PlatformInstitute of Forensic ScienceMinistry of JusticePRCShanghaiChina Pharmacy School of Wenzhou Medical University WenzhouChina

Acute fatal poisoning due to the inhalation of toxic gas frequently occurs in *** sulphur compounds(VSCs)are toxic to *** fatal poisoning investigations,such as those in industrial settings,a number of VSCs,including methanethiol(MT),dimethyl sulphide(DMS),dimethyl disulphide(DMDS)and dimethyl trisulphide(DMTS),can *** date,there is limited data regarding these compounds in post-mortem *** the present study,we report toxicological findings in a fatal accident case with two *** gas chromatography/flame ionization detector with two columns of different polarities was utilized to screen MT,DMS,DMDS and DMTS in *** limits of detection in both methods were 0.05 mg/*** sulphur compounds were detected in the blood samples of the two *** and DMDS were detected in the lungs at concentrations of 0.5 and 1.3 mg/g and 2.2 and 4.1 mg/g,*** liver concentrations were 2.5 and 6.5 mg/*** addition to hydrogen sulphide,screening for additional VSCs could help establish the cause of death.

关键词： forensic science forensic toxicology volatile sulphur compounds HS-GC/FID screening fatal accident case

Detecting genetic hypermutability of gastrointestinal tumor by using a forensic STR kit

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Frontiers of Medicine 2020年第1期14卷 101-111页

作者： Anqi Chen Suhua Zhang Jixi Li Chaoneng Ji Jinzhong Chen Chengtao Li State key laboratory of Genetic Engineering Institute of GeneticsSchool of Life SciencesFudan UniversityShanghai 200433China Shanghai key laboratory of forensic Medicine Shanghai Forensic Service PlatformInstitute of Forensic SciencesMinistry of JusticeShanghai 200063China

Growing evidence suggests that somatic hypermutational status and programmed cell death-1 overexpression are potential predictive biomarkers indicating treatment benefits from immunotherapy using immune checkpoint ***,biomarker-matched trials are still limited,and many of the genomic alterations remain difficult to *** isolate the potential somatic hypermutational tumor from microsatellite instability low/microsatellite stability(MSI-L/MSS)cases,we employed two commercial kits to determine MSI and forensic short tandem repeat(STR)alternations in 250 gastrointestinal(GI)*** types of forensic STR alternations,namely,allelic loss,Aadd,and Anew,were identified.62.4%(156/250)of the patients with GI exhibited STR alternation,including 100%(15/15)and 60%(141/235)of the microsatellite high instability and MSI-L/MSS cases,respectively.30%(75/250)of the patients exhibited STR instability with more than 26.32%(26.32%–84.21%)STR *** cutoff with 26.32%of the STR alternations covered all 15 MSI cases and suggested that it might be a potential *** the similar mechanism of the mutations of MSI and forensic STR,the widely used forensic identifier STR kit might provide potential usage for identifying hypermutational status in GI cancers.

关键词： mismatch repair protein deficiency(MMR-D) microsatellite instability(MSI) short tandem repeats(STR) gastrointestinal tumor hypermutability

Major depressive disorder:hypothesis,mechanism,prevention and treatment

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Signal Transduction and Targeted Therapy 2024年第3期9卷 913-944页

作者： Lulu Cui Shu Li Siman Wang Xiafang Wu Yingyu Liu Weiyang Yu Yijun Wang Yong Tang Maosheng Xia Baoman Li Department of forensic Analytical toxicology School of Forensic MedicineChina Medical UniversityShenyangChina Liaoning Province key laboratory of forensic Bioevidence Sciences ShenyangChina China Medical University Centre of forensic Investigation ShenyangChina International Joint Research Centre on Purinergic Signalling/key laboratory of Acupuncture for Senile Disease(Chengdu University of TCM) Ministry of Education/School of Health and RehabilitationChengdu University of Traditional Chinese Medicine/Acupuncture and Chronobiology Key Laboratory of Sichuan ProvinceChengduChina Department of Orthopaedics The First HospitalChina Medical UniversityShenyangChina

Worldwide,the incidence of major depressive disorder(MDD)is increasing annually,resulting in greater economic and social ***,the pathological mechanisms of MDD and the mechanisms underlying the effects of pharmacological treatments for MDD are complex and unclear,and additional diagnostic and therapeutic strategies for MDD still are *** currently widely accepted theories of MDD pathogenesis include the neurotransmitter and receptor hypothesis,hypothalamicpituitary-adrenal(HPA)axis hypothesis,cytokine hypothesis,neuroplasticity hypothesis and systemic influence hypothesis,but these hypothesis cannot completely explain the pathological mechanism of *** it is still hard to adopt only one hypothesis to completely reveal the pathogenesis of MDD,thus in recent years,great progress has been made in elucidating the roles of multiple organ interactions in the pathogenesis MDD and identifying novel therapeutic approaches and multitarget modulatory strategies,further revealing the disease features of ***,some newly discovered potential pharmacological targets and newly studied antidepressants have attracted widespread attention,some reagents have even been approved for clinical treatment and some novel therapeutic methods such as phototherapy and acupuncture have been discovered to have effective improvement for the depressive *** this work,we comprehensively summarize the latest research on the pathogenesis and diagnosis of MDD,preventive approaches and therapeutic medicines,as well as the related clinical trials.

关键词： prevention acupuncture hypothesis

PBPK modeling and simulation in drug research and development

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Acta Pharmaceutica Sinica B 2016年第5期6卷 430-440页

作者： Xiaomei Zhuang Chuang Lu State key laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and Toxicology Department of DMPK BiogenInc.

Physiologically based pharmacokinetic(PBPK) modeling and simulation can be used to predict the pharmacokinetic behavior of drugs in humans using preclinical *** can also explore the effects of various physiologic parameters such as age,ethnicity,or disease status on human pharmacokinetics,as well as guide dose and dose regiment selection and aid drug–drug interaction risk *** modeling has developed rapidly in the last decade within both the field of academia and the pharmaceutical industry,and has become an integral tool in drug discovery and *** this mini-review,the concept and methodology of PBPK modeling are briefly *** case studies were discussed on how PBPK modeling and simulation can be utilized through various stages of drug discovery and *** case studies are from our own work and the literature for better understanding of the absorption,distribution,metabolism and excretion(ADME) of a drug candidate,and the applications to increase efficiency,reduce the need for animal studies,and perhaps to replace clinical *** regulatory acceptance and industrial practices around PBPK modeling and simulation is also discussed.

关键词： PBPK PK prediction Absorption Metabolism Drug–drug interaction Special population

Implications of alpha-synuclein nitration at tyrosine 39 in methamphetamine-induced neurotoxicity in vitro and in vivo

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Neural Regeneration Research 2019年第2期14卷 319-327页

作者： Hong-Hua Qiao Lin-Nan Zhu Yue Wang Jia-Liang Hui Wei-Bing Xie Chao Liu Ling Chen Ping-Ming Qiu School of forensic Medicine Southern Medical University Kingmed Institute for forensic Science First Clinical Medicine College Southern Medical University Guangzhou forensic Science Institute Guangdong Province Key Laboratory of Forensic Genetics

Methamphetamine is an amphetamine-type psychostimulant that can damage dopaminergic neurons and cause characteristic pathological changes similar to neurodegenerative diseases such as Parkinson's disease. However, its specific mechanism of action is still unclear. In the present study, we established a Parkinson's disease pathology model by exposing SH-SY5 Y cells and C57 BL/6 J mice to methamphetamine. In vitro experiments were performed with 0, 0.5, 1.0, 1.5, 2.0 or 2.5 mM methamphetamine for 24 hours or 2.0 mM methamphetamine for 0-, 2-, 4-, 8-, 16-, and 24-hour culture of SH-SY5 Y cells. Additional experimental groups of SH-SY5 Y cells were administered a nitric oxide inhibitor, 0.1 mM N-nitro-L-arginine, 1 hour before exposure to 2.0 mM methamphetamine for 24 hours. In vivo experiments: C57 BL/6 J mice were intraperitoneally injected with N-nitro-L-arginine(8 mg/kg), eight times, at intervals of 12 hours. Methamphetamine 15 mg/kg was intraperitoneally injected eight times, at intervals of 12 hours, but 0.5-hour after each N-nitro-L-arginine injection in the combined group. Western blot assay was used to determine the expression of nitric oxide synthase, α-synuclein(α-Syn), 5 G4, nitrated α-synuclein at the residue Tyr39(nT39 α-Syn), cleaved caspase-3, and cleaved poly ADP-ribose polymerase(PARP) in cells and mouse brain tissue. Immunofluorescence staining was conducted to measure the positive reaction of NeuN, nT39 α-Syn and 5 G4. Enzyme linked immunosorbent assay was performed to determine the dopamine levels in the mouse brain. After methamphetamine exposure, α-Syn expression increased; the aggregation of α-Syn 5 G4 increased; nT39 α-Syn, nitric oxide synthase, cleaved caspase-3, and cleaved PARP expression increased in the cultures of SH-SY5 Y cells and in the brains of C57 BL/6 J mice; and dopamine levels were reduced in the mouse brain. These changes were markedly reduced when N-nitro-L-arginine was administered with methamphetamine in both SH-SY5 Y cells

关键词： nerve regeneration alpha-synuclein nitrated α-synuclein Parkinson's disease methamphetamine N-nitro-L-arginine alpha-synuclein aggregation apoptosis neurotoxicity neural regeneration

Engineered microneedles arrays for wound healing

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Engineered Regeneration 2022年第3期3卷 232-240页

作者： Shun Yao Yuan Luo Yongan Wang State key laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China

Wound healing is the regenerative process of original skin structure after destructing by different damage *** to their transdermal delivery capability and high specific surface area,microneedles arrays(MAs)have been recognized as encouraging biomaterials for wound *** this review,we have outlined the engineered MAs used for tissue regeneration and wound *** MAs were first classified by design methodologies such as bionic design,intelligent-responsive design,actively-triggered design,matrix materials innovation,and composite smart ***,the MAs were divided into two categories based on the different loading substances:drug-loaded MAs and living component-loaded ***,we have summed up the important elements of the preceding discussions and forecasted their future evolution.

关键词： Engineered design Microneedles arrays Wound healing